An updated patent review of SOS1 inhibitors (2022-present)
文献类型：期刊论文
| 作者 | Zhou, Guizhen5,6; Zhou, Chuan4; Ma, Xinyi3,5; Xu, Jiahang1,2,5; Zhou, Zehui4; Xu, Tianfeng2,3,4; Zheng, Mingyue1,2,3,5 ; Zhang, Sulin2,5
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| 刊名 | EXPERT OPINION ON THERAPEUTIC PATENTS
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| 出版日期 | 2024-10-27 |
| 页码 | 15 |
| 关键词 | SOS1 KRAS cancer inhibitor drug discovery |
| ISSN号 | 1354-3776 |
| DOI | 10.1080/13543776.2024.2419825 |
| 英文摘要 | IntroductionSOS1 is a crucial guanine nucleotide exchange factor for KRAS. It facilitates the transition of KRAS from inactive GDP-bound state to active GTP-bound state. The activation of KRAS triggers downstream signaling pathways, promoting tumor initiation and progression. Inhibiting SOS1 to prevent KRAS activation is an effective strategy for treating tumors driven by KRAS.Areas coveredThis review identified patents claiming to be SOS1 inhibitors or SOS1-KRAS interaction modulators published between January 2022 and June 2024 using Cortellis Drug Discovery Intelligence. A total of 15 patent applications from 5 different applicants were assessed.Expert opinionsIn KRAS-driven tumors, inhibiting SOS1 significantly affect cell proliferation and migration by modulating the RAS/MAPK and PI3K/AKT/mTOR signaling pathways. Since 2022, numerous patents for SOS1 inhibitors have been published. The majority of SOS1 inhibitors are currently in the preclinical phase of development, with only a few progressing to clinical trials. However, these inhibitors face significant challenges in clinical studies, including limited efficacy of monotherapies, safety concerns, and the necessity to enhance PK properties. Despite their excellent in vitro performance, SOS1 inhibitors must address issues related to safety, pharmacokinetics, and pharmacodynamics in clinical applications. |
| WOS关键词 | NEGATIVE FEEDBACK-REGULATION ; TARGETING SON ; SEVENLESS 1 ; RAS ; CANCER ; MUTATIONS ; SWITCH ; KRAS |
| 资助项目 | National Natural Science Foundation of China[T2225002] ; National Natural Science Foundation of China[82273855] ; National Key Research and Development Program of China[2022YFC3400504] ; Youth Innovation Promotion Association CAS[2023296] ; Natural Science Foundation of Shanghai[22ZR1474300] ; Natural Science Foundation of Shanghai[20ZR1468500] |
| WOS研究方向 | Pharmacology & Pharmacy |
| WOS记录号 | WOS:001341224000001 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/314306]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Xu, Tianfeng; Zheng, Mingyue; Zhang, Sulin |
| 作者单位 | 1.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou, Peoples R China 2.Univ Chinese Acad Sci, Beijing, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 5.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 6.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhou, Guizhen,Zhou, Chuan,Ma, Xinyi,et al. An updated patent review of SOS1 inhibitors (2022-present)[J]. EXPERT OPINION ON THERAPEUTIC PATENTS,2024:15. |
| APA | Zhou, Guizhen.,Zhou, Chuan.,Ma, Xinyi.,Xu, Jiahang.,Zhou, Zehui.,...&Zhang, Sulin.(2024).An updated patent review of SOS1 inhibitors (2022-present).EXPERT OPINION ON THERAPEUTIC PATENTS,15. |
| MLA | Zhou, Guizhen,et al."An updated patent review of SOS1 inhibitors (2022-present)".EXPERT OPINION ON THERAPEUTIC PATENTS (2024):15. |
入库方式： OAI收割
来源：上海药物研究所
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